Glycopeptide antibiotics are a class of antibiotic drugs which include glycosylated cyclic or polycyclic nonribosomal peptides. Examples include vancomycin, teicoplanin, telavancin, bleomycin, ramoplanin, and decaplanin.
Glycopeptide antibiotics inhibit the synthesis of cell walls in susceptible microbes by inhibiting peptidoglycan synthesis. The compounds bind to the amino acids within the cell wall preventing the addition of new units to the peptidoglycan. In particular, the compounds bind to acyl-D-alanyl-D-alanine in peptidoglycan.
Due to their toxicity, use of glycopeptide antibiotics is restricted to patients who are critically ill, who have a demonstrated hypersensitivity to the 3-lactams, and/or who are infected with β-lactam-resistant species. These antibiotics are effective principally against Gram-positive cocci. They exhibit a narrow spectrum of action, and are bacteriocidal only against the enterococci. Glycopeptide antibiotics continue to be one of the last effective lines of defense for cases of Methicillin-resistant Staphylococcus aureus (MRSA). However, vancomycin-resistant enterococci (VRE) and Vancomycin-resistant staphylococcus aureus (VRSA) has been seen in some countries.
There exists a need for derivatives of glycopeptide antibiotics which are effective at treating vancomycin-susceptible or vancomycin resistant enterococci or Staphylococcus aureus. 
Therefore, it is an object of the invention to provide derivatives of glycopeptide antibiotics which are effective at treating vancomycin-susceptible or vancomycin resistant enterococci or Staphylococcus aureus, and methods of making and using thereof.